1. Technical Field
This invention concerns topical formulations and, more particularly, topical skin protectant formulations that can be sprayed.
2. Background
Drugs and other substances are often applied to human skin to protect it from harmful stimuli. The U.S. Food And Drug Administration (“FDA”) has in the past defined a “skin protectant” as a drug that protects injured or exposed skin or mucous membrane surfaces from harmful or annoying stimuli (21 CFR §347.3 (1983)). Thus, a “skin protectant” can be used to protect and/or treat skin in connection with various indications, including diaper rash; minor burns; cuts; scrapes; sunburn; chaffed, chapped, cracked, or windburned skin or lips; skin irritation; and oozing and/or weeping of skin caused by poison ivy, poison oak, and/or poison sumac.
The skin of infants is known to be highly sensitive, particularly to chemical substances. One common skin problem of infants is diaper dermatitis, more commonly called “diaper rash.” “Diaper rash” has been defined by the FDA as an inflammatory skin condition in the diaper area (perineum, buttocks, lower abdomen, and inner thighs) caused by one or more of the following factors: moisture, occlusion, chaffing, continued contact with urine or feces or both, or mechanical or chemical irritation (21 CFR §347.3 (1990)), and that definition will be used herein. The FDA has also indicated that mild diaper rash appears as simple erythema and that more severe conditions may be accompanied by papules, vesicles, oozing, and ulceration. Adults (e.g., incontinent adults) may also suffer from diaper rash.
Strategies for dealing with diaper rash include removing the source of irritation, reducing the immediate skin reaction, relieving discomfort, and preventing secondary infection. Many products used in treating diaper rash are designed to provide a barrier between the skin and the waste products. Known barrier ingredients include zinc oxide and petrolatum. Barrier products containing oily substances such as petrolatum may feel greasy, may be difficult to apply because of their high viscosity, and may not be easily removed from hands that apply the products or from the infant's skin. Clean-up of these products from the hands and from the infant's skin may be regarded by some as time-consuming, messy, and inconvenient.
The FDA will allow claims to be made that the following substances are useful as skin protectants provided, among other things, that those substances are used at FDA-specified concentration levels: mineral oil, dimethicone, zinc oxide, allantoin, calamine, kaolin, petrolatum, white petrolatum, cod liver oil, lanolin, talc, topical starch, aluminum hydroxide gel, cocoa butter, glycerine, shark liver oil, zinc acetate, and zinc carbonate, all of which will be referred to herein as “active ingredients for protecting skin” (21 CFR §347.10 (1983 and 1990)). As used herein, the terms “protecting skin,” “protecting the skin,” and “protecting human skin” are synonymous and each include protecting and/or treating skin in connection with various indications involving the skin, including diaper rash; minor burns; cuts; scrapes; sunburn; chaffed, chapped, cracked, or windburned skin or lips; skin irritation; and oozing and/or weeping of skin caused by poison ivy, poison oak, and/or poison sumac.
The FDA will allow claims to be made that the following substances are useful in treating diaper rash provided, among other things, that those substances are used at FDA-specified concentration levels: mineral oil, dimethicone, zinc oxide, allantoin, calamine, kaolin, petrolatum, white petrolatum, cod liver oil, lanolin, talc, and topical starch, all of which will be referred to herein as “active ingredients for treating diaper rash” (21 CFR §347.10 (1983 and 1990)). For example, assuming all the other requirements are met, the FDA will allow a claim to be made that a composition containing dimethicone is useful for treating diaper rash if the dimethicone concentration is from 1% w (percent by weight) to 30% w. A similar claim can be made for a composition containing zinc oxide if the zinc oxide concentration is from 1% w to 40% w. A similar claim can be made for a composition containing mineral oil if the mineral oil concentration is from 50% w to 100% w. As used herein, the term “treating diaper rash” includes treating an existing diaper rash condition or preventing a diaper rash condition or both.
Compositions that may contact the skin and may contain zinc oxide, and/or mineral oil, and/or silicon dioxide (silica), and/or dimethicone or other silicone compounds, some of which compositions may be in the form of aerosols or sprays and some of which compositions may be used for treating diaper rash, include those compositions referred to in U.S. Pat. Nos. Re. 33,107, 2,843,522, 3,770,648, 3,935,862, 4,043,077, 4,196,218, 4,273,786, 4,278,658, 4,329,366, 4,389,418, 4,514,383, 4,556,560, 4,569,839, 4,574,082, 4,672,074, 4,725,438, 4,800,076, 4,816,254, 4,842,593, 4,847,071, 4,911,932, 4,933,330, 4,938,960, 4,996,238, 4,996,239, 5,043,359, 5,085,856, 5,137,714, 5,208,031, 5,210,102, 5,232,691, 5,234,689, 5,266,318, 5,362,488, 5,389,204, 5,436,007, 5,527,519, 5,543,135, 5,545,673, 5,558,872, 5,573,753, 5,576,006, 5,603,863, 5,616,331, 5,635,191, 5,643,588, 5,652,274, 5,662,937, 5,665,426, 5,730,993, 5,733,895, 5,744,146, 5,756,082, 5,756,110, 5,762,945, 5,776,440, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,869,061, 5,869,062, 5,869,071, 5,874,094, 5,885,599, 5,914,101, 5,939,053, 5,945,211, 5,958,397, 5,961,961, 5,962,441, 5,965,137, 5,965,610, 5,968,531, and 5,972,359. (All of the these documents and any other documents discussed or otherwise referenced or identified herein are incorporated herein in their entireties for all purposes.)
Compositions containing zinc oxide that may contact the skin include those referred to in U.S. Pat. Nos. 2,843,522, 3,770,648, 4,034,077, 4,278,658, 4,389,418, 4,556,560, 4,569,839, 4,672,074, 4,816,254, 4,911,932, 4,933,330, 5,085,856, 5,208,031, 5,232,691, 5,527,519, 5,543,135, 5,545,673, 5,573,753, 5,603,863, 5,616,331, 5,652,274, 5,662,937, 5,665,426, 5,730,993, 5,733,895, 5,744,146, 5,756,110, 5,762,945, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,869,062, 5,874,094, 5,885,599, 5,914,101, 5,939,053, 5,945,211, 5,961,961, 5,962,441, 5,965,610, 5,968,531, and 5,972,359.
Some of the compositions containing zinc oxide may be sprayable (with or without a propellant). See, e.g., U.S. Pat. Nos. 3,770,648, 4,278,658, 4,933,330, 5,652,274, 5,733,895, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,885,599, 5,939,053, 5,945,211, 5,962,441, 5,965,610, and 5,972,359.
Some of the compositions containing zinc oxide may contain small zinc oxide particles (e.g., less than 1 micron). See, e.g., U.S. Pat. Nos. 5,543,135, 5,527,519, 5,573,753, 5,603,863, 5,616,331, 5,730,993, 5,756,110, 5,861,143, 5,861,144, 5,861,146, 5,914,101, 5,945,211, 5,961,961, and 5,972,359.
Topical compositions for treating diaper rash containing zinc oxide include DESITIN® Ointment and DESITIN® Creamy Ointment, both marketed by Pfizer Inc, the assignee of the present application. DESITIN® Ointment contains about 40% w zinc oxide and other ingredients, including white petrolatum, cod liver oil, lanolin, talc, and about 5% w water. DESITIN® Creamy Ointment contains about 10% w zinc oxide and other ingredients, including mineral oil, mineral wax, dimethicone, cyclomethicone, white petrolatum, white wax, and over 30% w water.
Other diaper rash, incontinence/dermatitis, diaper-treating, and baby treatment compositions include those referred to in U.S. Pat. Nos. Re.33,107, 2,843,522, 3,770,648, 3,935,862, 4,034,077, 4,273,786, 4,329,366, 4,556,560, 4,816,254, 4,842,593, 4,911,932, 4,996,238, 4,996,239, 5,362,488, 5,436,007, 5,576,006, 5,558,872, 5,635,191, 5,643,588, 5,652,274, 5,762,945, 5,834,290, 5,869,071, and 5,945,211.
Some of those diaper rash, incontinence/dermatitis, diaper-treating, and baby treatment compositions may form a film when they are topically applied and may be resistant to wetting by moisture. See, e.g., U.S. Pat. No. 4,996,238 (column 2, line 20 and following) and U.S. Pat No. 4,996,239(column 2, line 40 and following).
Some of those diaper rash, incontinence/dermatitis, diaper-treating, and baby treatment compositions may contain film-forming agents. See, e.g., U.S. Pat. No. 4,996,238 (column 2, line 42 and following), U.S. Pat. No. 4,996,239 (column 2, line 63 and following), U.S. Pat. No. 5,635,191 (column 18, line 34), and U.S. Pat. No. 5,643,588 (column 18, line 47).
Some of those diaper rash, incontinence/dermatitis, diaper-treating, and baby treatment compositions may be sprayable (with or without a propellant). See, e.g., U.S. Pat. Nos. Re.33,107, 3,770,648, 3,935,862, 4,273,786, 4,329,366, 4,842,593, 5,436,007, 5,576,006, 5,635,191, 5,643,588, 5,652,274, 5,869,071, and 5,945,211.
U.S. Pat. No. Re. 33,107 refers to sprays that may contain mineral oil for treating skin conditions such as dermatitis.
U.S. Pat. No. 3,770,648, assigned on its face to Bristol-Myers Company, refers to substantially non-aqueous quick-breaking aerosol foaming compositions containing silicone compounds (e.g., dimethyl silicone fluids), foamable organic liquids (e.g., mineral oil), and a high vapor pressure propellant system (e.g., fluorocarbons). Example 2 of the patent refers to what is called “DESITIN® baby foam,” containing zinc oxide (about 4.2% w), mineral oil (about 71.7% w), a silicone, and FREON 12 fluorocarbon propellant.
U.S. Pat. Nos. 3,935,862 and 4,273,786 refer to compositions containing amino acid compounds to inhibit the formation of ammonia and therefore treat diaper rash. The compositions may contain solid diluents such as starch and talc and may also contain silicone-type fluids such as polysiloxane fluid. Although mineral oil is referred to in some of the non-sprayable compositions exemplified in the patents, the only sprayable composition (Example H) contains micropulverized talc, an amino acid salt, fragrance, anhydrous ethanol, isopropyl myristate, and two FREON propellants.
U.S. Pat. No. 4,329,366 refers to compositions containing acylaminophenols that can be used to treat various conditions, including diaper rash. Although mineral oil is referred to in some of the non-sprayable formulations exemplified, the two sprayable formulations (Formulations F and L) use alcohol and propellants and at least one of them (Formulation F) contains water.
U.S. Pat. No. 4,842,593 refers to a pH control system that can be sprayed onto an article used to prevent or reduce diaper rash. The fibers of the article may be impregnated with silica.
U.S. Pat. No. 5,436,007 refers to a diaper rash lotion that may be sprayed containing dimethicone (e.g., from 1% w to 30% w), water (e.g., from 50% w to 95% w), and an emulsifier (e.g., from 1% w to 10% w). The patent also refers to a diaper rash cream that may contain a linear polydimethylsiloxane (e.g., 20% w), a light mineral oil (e.g., 4% w), emulsifier (e.g., 8% w), and water (e.g., over 40% w). Stearic acid, which is said to function as a thickener, and aloe may also be used in the lotion and the cream. See, e.g., column 7, line 6, to column 10, line 26.
U.S. Pat. No. 5,576,006 refers to antibacterial compositions that can be used to deodorize footwear and to treat diaper rash. Although the footwear deodorizing compositions can be sprays, it appears that the compositions intended for use on infants are “body preparations and powders,” which may contain talc (column 3, lines 47-63, and Example 3). The sprays exemplified contain water.
U.S. Pat. Nos. 5,635,191 and 5,643,588 refer to a diaper having a topsheet coated with a composition containing emollients (such as mineral oil, petrolatum or mineral wax, and polysiloxanes) and other ingredients (such as viscosity modifiers and film formers). The composition may be sprayed onto the topsheet. According to the patents, the composition on the diaper topsheet is transferred to the wearer's skin and those topsheets provide “BM [bowel movement] cleaning, therapeutic or protective lotion coating benefits” (U.S. Pat. No. 5,635,191, column 2, line 64, to column 3, line 52; and U.S. Pat. No. 5,643,588, column 2, line 62, to column 3, line 51). The composition is “solid” or “semisolid” at 20 degrees Centigrade (U.S. Pat. No. 5,635,191, column 9, lines 35-67; and U.S. Pat. No. 5,643,588, column 9, line 39, to column 10, line 4) and is “substantially free of water” (U.S. Pat. No. 5,635,191, column 10, lines 43-54, and U.S. Pat. No. 5,643,588, column 10, lines 48-59).
U.S. Pat. No. 5,652,274 refers to therapeutic wound healing compositions. Compositions for treating diaper dermatitis are discussed, for example, at column 11, lines 31-49; column 15, lines 39-61; column 26, lines 5-26; and column 138, line 52, to column 145, line 4. Those compositions may contain zinc oxide. At least some compositions may be sprayed (for example, the formulations of Embodiment One; see column 42, line 26). Some of the compositions may contain petrolatum, mineral oil, and vitamin E (see, e.g., column 66, lines 35-49).
U.S. Pat. No. 5,869,071 refers to a spray composition for incontinent patients that “cleanses, moisturizes and leaves a protective petrolatum barrier against wetness and irritants in one step” (column 1, lines 58-63). The composition is said to be an emulsion of water and petrolatum (or petroleum jelly) and may contain dimethicone, cyclomethicone, mineral oil, vitamin E, and aloe.
U.S. Pat. No. 5,945,211 refers to a composite to which zinc oxide particles are adhered. The composite may be a diaper and the zinc oxide may be deposited on the composite from an aqueous medium (e.g., by spraying an aqueous suspension of zinc oxide).
Sprayable (with or without a propellant) compositions that may contact the skin and that may contain dimethicone or other silicon compounds include those referred to in U.S. Pat. Nos. 3,770,648, 3,935,862, 4,273,786, 4,514,383, 4,847,071, 4,933,330, 5,137,714, 5,266,318, 5,389,204, 5,436,007, 5,635,191, 5,643,588, 5,733,895, 5,776,440, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,869,071, 5,885,599, 5,939,053, 5,962,441, 5,965,610, and 5,972,359.
Compositions containing some form of silica (silicon dioxide) include those referred to in U.S. Pat. Nos. 4,574,082, 4,800,076, 4,996,238, 4,996,239, 5,137,714, 5,208,031, 5,527,519, 5,543,135, 5,573,753, 5,603,863, 5,616,331, 5,733,895, 5,756,082, 5,756,110, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,885,599, 5,914,101, 5,939,053, 5,968,531, and 5,972,359. Some forms of silica are said to be useful as thickeners. See, e.g., U.S. Pat. Nos. 4,996,238 and 4,996,239.
Some of those compositions containing some form of silica also may contain zinc oxide. See, e.g., U.S. Pat. Nos. 5,208,031, 5,527,519, 5,543,135, 5,573,753, 5,603,863, 5,616,331, 5,733,895, 5,756,110, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,885,599, 5,914,101, 5,939,053, 5,968,531, and 5,972,359.
Some of those compositions containing silica (with or without zinc oxide) may be sprayable. See, e.g., U.S. Pat. Nos. 5,137,714, 5,733,895, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,885,599, 5,939,053, and 5,972,359.
Some sprayable compositions may contain aloe and/or a form of vitamin E. See, e.g., U.S. Pat. Nos. 4,847,071, 5,266,318, 5,436,007, 5,861,143, 5,861,144, 5,861,146, 5,869,071, 5,885,599, 5,965,137, 5,965,610, and 5,972,359. Some of the composition containing aloe and/or a form of vitamin E may be for treating diaper rash and/or incontinence/dermatitis. See, e.g., U.S. Pat. Nos. 5,436,007 and 5,869,071.
Compositions containing (a) mineral oil or petrolatum, (b) zinc oxide, and (c) dimethicone or other silicone ingredient include those referred to in U.S. Pat. Nos. 3,770,648, 4,389,418, 4,556,560, 4,569,839, 4,911,932, 4,933,330, 5,085,856, 5,208,031, 5,232,691, 5,543,135, 5,603,863, 5,616,331, 5,665,426, 5,730,993, 5,733,895, 5,744,146, 5,756,110, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,885,599, 5,914,101, 5,939,053, 5,961,961, 5,962,441, 5,965,610, and 5,972,359. Some of those compositions may be sprayable (with or without a propellant). See, e.g., U.S. Pat. Nos. 3,770,648, 4,933,330, 5,733,895, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,885,599, 5,939,053, 5,962,441, 5,965,610, and 5,972,359. Some of those compositions may be for treating diaper rash. See, e.g., U.S. Pat. Nos. 4,556,560 and 4,911,932.
Some of those compositions containing (a) mineral oil or petrolatum, (b) zinc oxide, and (c) dimethicone or other silicone ingredient may also contain silica. See, e.g., U.S. Pat. Nos. 5,208,031, 5,543,135, 5,603,863, 5,616,331, 5,733,895, 5,756,110, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,885,599, 5,914,101, 5,939,053, and 5,972,359. Some of those compositions may be sprayable (with or without a propellant). See, e.g., U.S. Pat. Nos. 5,733,895, 5,834,290, 5,861,143, 5,861,144, 5,861,146, 5,863,522, 5,885,599, 5,939,053, and 5,972,359.
Some of those compositions containing (a) mineral oil or petrolatum, (b) zinc oxide, and (c) dimethicone or other silicone ingredient may also contain wax. See, e.g., U.S. Pat. Nos. 4,389,418, 4,556,560, 4,569,839, 4,911,932, 4,933,330, 5,085,856, 5,208,031, 5,232,691, 5,616,331, 5,665,426, 5,730,993, 5,733,895, 5,744,146, 5,834,290, 5,863,522, 5,939,053, and 5,961,961. Some of those compositions may be sprayable (with or without a propellant). See, e.g., U.S. Pat. Nos. 4,933,330, 5,733,895, 5,834,290, 5,863,522, and 5,939,053.
Despite all the work done in this technical area, the need still exists for a safe and effective liquid skin protectant composition that is liquid, is water-repellent, substantially anhydrous, can be applied directly to the skin, quickly, easily, and without messing one's hands with the composition, and that will not run after it has been applied to the skin. Moreover, the need still exists for such a composition that can be applied to the skin without the need to use high-pressure such as that provided by propellant gas in an aerosol can. Furthermore, the need still exists for a composition meeting all those criteria that can be used for treating diaper rash.